Description: Nolatrexed dihydrochloride (Thymitaq) is the dihydrochloride salt of nolatrexed, a water-soluble lipophilic quinazoline folate analog with antineoplastic activity. Nolatrexed occupies the folate binding site of thymidylate synthase, resulting in inhibition of thymidylate synthase activity and thymine...

Nolatrexed is a thymidylate synthase inhibitor (Ki = 11 nM). It inhibits cell growth in a panel of human and murine cancer cell lines (IC50s = 0.39-6.6 µM). Nolatrexed inhibits the growth of L1210 cells, an effect that is decreased by greater than 50-fold by the addition of exogenous thymidine. Nolatrexed (0.7 and...